Complete information including dosage, side effects, interactions and pregnancy & breast feeding warnings for patient and professional use

Overview and uses

Busulfan is an alkylating agent used for the treatment of cancer.

Indication (uses)

  • Used in combination with cyclophosphamide as a conditioning regimen prior to allogeneic hematopoietic progenitor cell transplantation for chronic myelogenous leukemia (injection).
  • Used for the palliative treatment of chronic myelogenous (myeloid, myelocytic, granulocytic) leukemia (tablets).

Pharmacological classification

Alkylating agent used for the treatment of cancer.

Brand names


Dosage form

  • Supplied as 10 ml single use vial containing Busulfan 60 mg in a concentration of 6 mg/ml.
  • Supplied as scored tablets containing 2 mg of Busulfan.

Mechanism of action

Alkylating agents produce highly reactive carbonium ion intermediates which transfer alkyl groups to cellular macromolecules by forming covalent bonds. These intermediates may react with carboxyl, hydroxyl, amino, sulfhydryl and phosphate groups of biomacromolecules. Alkylation results in cross linking/abnormal base pairing/scission of DNA strand. Cross linking of nucleic acids with proteins can also take place.


  • Injection
    • 8 mg/kg of ideal body weight or actual body weight.
    • Busulfan is administered as a two hour infusion every 6 hours for 4 consecutive days for a total of 16 doses.
    • Further instructions regarding Busulfan injection
      • Busulfan should be administered in combination with cyclophosphamide 60 mg/kg.
      • Cyclophosphamide should be administered intravenously as a 1 hour infusion on each of 2 days beginning no sooner than 16 hours following the 16th dose of Busulfan.
      • Patients should be premedicated with anticonvulsants, 12 hours before the first dose and 24 hours after the last dose.
      • Manufacturer states that use of polycarbonate syringes or polycarbonate filter needles should be avoided with Busulfan.
    • Tablets
      • Initial dose
        • 60 mcg/kg of body weight or 1.8 mg/m2 of body surface area.
      • Adult dose for remission induction
        • 4 mg to 8 mg daily.

Renal dose adjustments

  • Data not available.

Hepatic dose adjustments

  • Data not available.

Other dose adjustments

  • Consider dose adjustments in obese patients as Busulfan clearance increases in obese patients.
  • This adjustment should be done as suggested by Gibbs – ideal body weight + 25% of difference between actual and ideal body weight.


  • No specific antidote is known.
  • Dialysis should be considered in case of Overdosage.
  • Symptoms of Overdosage includes
  • Bone marrow hypoplasia/aplasia
  • pancytopenia
  • Treatment of overdosage involves
  • General supportive measures.

Side effects or adverse effects

  • Local side effects
    • Thrombophlebitis and thrombosis at the site of injection.
  • Hypersensitivity reactions
    • Anaphylaxis has been reported with Mechlorethamine use.
    • Pain in chest or abdomen, skin rash, difficulty in breathing, rapid breathing, shortness of breath, dizziness, fainting, low blood pressure are some of the symptoms.
    • Consult your doctor as soon as possible.
  • Myelosuppression
    • Severe granulocytopenia
    • Thrombocytopenia
    • Anemia
    • Reduction in absolute neutrophil count.
  • Seizures
    • Initiate phenytoin or any other anti convulsant prophylaxis therapy.
  • Hepato veno-occlusive disease
  • Bronchopulmonary dysplasia
    • Onset of symptoms is 4 years after therapy.
    • Bronchopulmonary dysplasia with pulmonary fibrosis is rare but serious complication.
  • Cellular dysplasia
    • Giant, hyperchromatic nuclei have been reported in lymph nodes, pancreas, thyroid, adrenal glands, liver, lungs and bone marrow.
  • Cardiac temponade
    • Abdominal pain and vomiting proceeded in most of the patients.
  • Other systemic side effects
    • Jaundice
    • Vertigo
    • Tinnitus
    • Diminished hearing
    • Occurrence/precipitation of hemolytic anemia
  • Bone marrow depression
    • Bone marrow depression is the most serious side effect/toxicity. It is also a limiting factor for the dose. Infections and bleeding are the common complications.
    • Bone marrow depression results in granulocytopenia, agranulocytosis, thrombocytopenia and aplastic anemia.
    • Consult your doctor as soon as possible if you observe any of the below mentioned symptoms:
      • Sore throat
      • Chills
      • Sudden fever
      • Weakness in limbs
      • Mouth ulcers
      • Bleeding gums
      • Sore mouth
      • Fast heart rate
      • Low blood pressure
      • Sore gums
      • Skin abscesses
      • Rapid breathing
      • Rapid progression of infection of any organ
      • Rapid progression of Septicemia
    • Gastrointestinal side effects
      • Nausea and vomiting are commonly observed with anti-cancer medicines.
      • Mucositis – painful inflammation and ulceration of mucus membrane lining the digestive tract.
      • Diarrhea, shredding of mucosa and haemorrhage due to decreased rate of renewal of gastrointestinal mucosa lining.
    • Skin
      • Alopecia or hair loss.
      • Dermatitis
    • Oral side effects
      • Breaches during chewing.
      • Depression of immunity due to reduction in number of WBCs largely increases the risk of oral infections.
      • Bleeding gums
      • Rapid progression of dental caries.
    • Gonadal side effects
      • Infertility due to Oligozoospermia in males.
      • Impotence in males.
      • Loss or reduces sex drive.
      • Inhibition of ovulation in females
      • Amenorrhea in females.
      • Damage to germinal cells may lead to mutagenesis.
    • Lymphoreticular tissue
      • Lymphocytopenia (reduced number of lymphocytes)
      • Inhibition of lymphocyte function.
      • Suppression of immunity due to bone marrow depression and reduced lymphocyte function highly increases the risk of opportunistic infections like:
        • Candida and other infections causing deep mycosis.
        • Cytomegalo virus
        • Herpes zoster
        • Pneumocystis jiroveci
        • Toxoplasma
      • Fetal side effects
        • Use of anti-cancer medicines in pregnant women may cause fetal damage leading to:
          • Fetal death
          • Abortion
          • Teratogenesis
        • Renal side effects
          • Renal failure, Gout and Urate stones may develop in urinary tract.
        • Hyperuricemia
          • An elevated level of uric acid is common in leukemia and bulky lymphomas.
        • Please note: The side effects mentioned above are from the reported cases. However, side effects are not limited to above mentioned conditions and symptoms. Consult your doctor as soon as possible if you feel or observe any symptoms that you relate to your treatment.

Warnings & Precautions

  • Contra-indicated in patients with known hypersensitivity to Busulfan.
  • Contra-indicated in patients with known infectious disease.
  • Hematologic status of the patient must be determined before starting Busulfan therapy.
  • Patient should be monitored for bone marrow depression.

Pregnancy & breast feeding warnings


  • Category D, which means there is positive evidence of human fetal risk based on adverse reaction data from investigational or marketing experience or studies in humans, but potential benefits may warrant use of the drug in pregnant women despite potential risks.


  • It is not known whether Busulfan is excreted in human breast milk or not.
  • Since many drugs are excreted in milk and because of the potential for side effects in nursing infants, a decision should be made whether to discontinue drug or to discontinue nursing.


Drug – drug interactions

  • Itraconazole decreases the Busulfan clearance by 25%.
  • Phenytoin increases the Busulfan clearance by 15%.
  • Concomitant use of Busulfan with following drugs/medicines should be strictly avoided.
    • Adalimumab as it increases the risk of infections.
    • Use of acetaminophen within 72 hours before the start of therapy of Busulfan or during Busulfan treatment may reduce the clearance of Busulfan.
    • Busulfan – blood levels or side effects of Busulfan may be increased by Thiotepa.
    • Certolizumab as it increases the risk of infections.
    • Clozapine as it may lower the WBC count.
    • Deferiprone as it may lower the WBC count.
    • Etanercept as it increases the risk of infections.
    • Fingolimod as it increases the risk of infections.
    • Golimumab as it increases the risk of infections.
    • Infliximab as it increases the risk of infections.
    • Leflunomide as it increases the risk of infections.
    • Nalidixic acid as the combination may cause unusual bruising or bleeding, nausea, stomach pain, unusual weakness, low fever and loss of appetite.
    • Natalizumab as it increases the risk of infections.
    • Teriflunomide as it increases the risk of infections.
    • Thalidomide with Busulfan may increase the risk of unusual blood clots.
    • Tofacitinib as it increases the risk of infections.
    • Concomitant use of metronidazole with Busulfan may cause unusual bleeding or bruising, fever, chills, congestion, persistent cough, shortness of breath, stomach or joint pain, unusual fatigue, sudden weakness, decreased appetite or weight loss, diarrhea, dizziness, nausea, vomiting and confusion.

Click here to go to Busulfan forums.


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  • “Product information. BUSULFEX® (Busulfan).” GlaxoSmithKline.
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  • Clinical Oncological Society of Australia. Guidelines and recommendations for safe handling of antineoplastic agents. Med J Australia. 1983;1:426-428.
  • National Study Commission on Cytotoxic Exposure. Recommendations for handling cytotoxic agents. 1987. Available from Louis P. Jeffrey, Chairman, National Study Commission on Cytotoxic Exposure. Massachusetts College of Pharmacy and Allied Health Sciences, 179 Longwood Avenue, Boston, MA 02115.
  • Jones RB, Frank R, Mass T. Safe handling of chemotherapeutic agents: a report from the Mount Sinai Medical Center. CA-A Cancer J for Clin. 1983;33:258-263.
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By |2018-12-29T07:35:46+00:00April 26th, 2017|medicines|Comments Off on busulfan

About the Author:

B. Pharm (K.L.E. society's S.V.V. Patil College of Pharmacy, Bengaluru) M. Pharm (Maharishi Arvind Institute of Pharmacy, Jaipur)


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